Some pyrazoles derivatives: Potent carbonic anhydrase, -glycosidase, and cholinesterase enzymes inhibitors

Turkan F., Cetin A., TASLIMI P., GÜLÇİN İ.

ARCHIV DER PHARMAZIE, cilt.351, sa.10, 2018 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 351 Sayı: 10
  • Basım Tarihi: 2018
  • Doi Numarası: 10.1002/ardp.201800200
  • Dergi Adı: ARCHIV DER PHARMAZIE
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Anahtar Kelimeler: acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase, enzyme inhibition, substituted pyrazol-4-yl-diazene, INCLUDING NATURAL-PRODUCTS, GLUTATHIONE-S-TRANSFERASE, ALPHA-GLUCOSIDASE, 1ST SYNTHESIS, ACETYLCHOLINESTERASE, BUTYRYLCHOLINESTERASE, PROFILES, ANTIOXIDANT, BROMOPHENOLS, BENZENESULFONAMIDES
  • Atatürk Üniversitesi Adresli: Evet

Özet

A series of substituteed pyrazol-4-yl-diazene derivatives were found to be effective inhibitors against -glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with K-i values in the range of 33.72 +/- 7.93 to 90.56 +/- 27.52nM for -glycosidase, 1.06 +/- 0.16 to 9.83 +/- 0.74nM for hCA I, 0.68 +/- 0.12 to 7.16 +/- 1.14nM for hCA II, 44.66 +/- 10.06 to 78.34 +/- 17.83nM for AChE, and 50.36 +/- 13.88 to 88.36 +/- 20.03nM for BChE, respectively. Recently, inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances, such as diabetes, glaucoma, obesity, epilepsy, cancer, and neurodegenerative diseases.